1,2,3-三唑金(I)-三乙基膦营养物衍生物作为抗革兰氏阳性耐药病原体的新抗生素。

IF 2.5 4区医学 Q3 CHEMISTRY, MEDICINAL

Bioorganic & Medicinal Chemistry Letters Pub Date : 2025-05-14 DOI:10.1016/j.bmcl.2025.130276

Mathieu Michaut , Françoise Hoegy , Alexandre Steffen , Jean-Marie Contreras , Christophe Morice , Patrick Plésiat , Gaëtan L.A. Mislin

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引用次数: 0

摘要

细菌对抗生素耐药性的持续上升是开发全新抗菌分子的动力。以三乙基膦-金(I)叠氮化物和氨基酸、烟酸、生物素等炔烃功能化代谢物为原料，通过点击化学合成了新型有机金(I)抗菌化合物。所得有机金(I)化合物对革兰氏阳性病原菌（葡萄球菌、肠球菌和艰难梭菌）具有显著的抑制作用，但在使用的条件下（8 μg L-1最大值）对革兰氏阴性杆菌（如大肠杆菌）的生长没有抑制作用。

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1,2,3-Triazole‑gold(I)-triethylphosphine derivatives of nutrients as new antimicrobials against antibiotic resistant Gram-positive pathogens

The ongoing rise of bacterial resistance against antibiotics is an incentive to develop radically new antibacterial molecules. Innovative organo-gold(I) antibacterial compounds were synthesized by click chemistry with triethylphosphine‑gold(I) azides and alkyne-functionalized metabolites like amino acids, nicotinic acid and biotin. The resulting organo‑gold(I) compounds exhibited remarkable activities against a panel of Gram-positive pathogens (Staphyloccocus sp., Enterococcus sp. and Clostridium difficile) but failed to inhibit the growth of Gram-negative bacilli (e.g., Escherichia coli) under the conditions used (8 μg. mL⁻¹ maximum).

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来源期刊

Bioorganic & Medicinal Chemistry Letters 医学-医药化学

CiteScore

5.70

自引率

3.70%

发文量

463

审稿时长

27 days

期刊介绍： Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.